posted on 2022-08-18, 12:20authored byChanghuo Xu, Hang Zou, Lianrui Hu, Hanchen Shen, Herman H. Y. Sung, Haitao Feng, Ryan T. K. Kwok, Jacky W. Y. Lam, Lei Zheng, Ben Zhong Tang
The development of fluorescent probes based on the skeletal
structure
of small-molecule targeted anticancer drugs is promising for biomedical
applications because these probes generally show trackable fluorescence
and connatural bioactivity inherited from the parental anticancer
drugs. By mimicking a classic estrogen receptor (ER) antagonist, namely,
tamoxifen, we herein design and synthesize a photoactivatable luminogen
with aggregation-induced emission and medicinal benefits. The probe
is weakly emissive when it is selectively internalized by estrogen
receptor-positive cells. Under photoirradiation, its emission can
be turned on to report the intracellular distribution. The cell viability
assay suggests that the probe only exhibits cytotoxicity to ER-positive
cells but negligible cytotoxicity to ER-negative cells. This study
thus provides new access to targeted theranostic systems with photoactivity.